CAS 253870-02-9

5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid

Codes: SUNT-016, VORO-002

Application context (from source-drug indications)

Pancreatic neuroendocrine tumourSunitinib MalateRenal cell carcinomaSunitinib MalateGastrointestinal stromal tumourSunitinib MalateOsteosarcomaSunitinib MalateSarcomaSunitinib MalateLymphomaSunitinib MalateRenal cell carcinomaVorolanibDiabetic macular oedemaVorolanib湿性年龄相关性黄斑变性VorolanibDiabetic retinopathyVorolanib肾肿瘤VorolanibHepatic function declineVorolanib

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Sunitinib Malate	Tier B — Position early	-
Vorolanib	Tier C — Watch / trade	-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

Sunitinib MalateProcess routesteps: 8total yield: 1.7 kg

N1,N1-diethylethane-1,2-diamine→tert-butyl 3-oxobutanoate→N-(2-(diethylamino)ethyl)-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide→5-fluoroindolin-2-one→(S)-2-hydroxysuccinic acid→(E)-tert-butyl 2-(hydroxyimino)-3-oxobutanoate→ethyl 3-oxobutanoate→2-(tert-butyl) 4-ethyl 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate→ethyl 2,4-dimethyl-1H-pyrrole-3-carboxylate→ethyl 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylate→5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid

Sunitinib MalateOptimised routesteps: 8total yield: 0.6 g

N1,N1-diethylethane-1,2-diamine→N-(2-(diethylamino)ethyl)-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide→ethyl 3-oxobutanoate→ethyl 2,4-dimethyl-1H-pyrrole-3-carboxylate→ethyl 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylate→5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid→diethyl 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate→4-(ethoxycarbonyl)-3,5-dimethyl-1H-pyrrole-2-carboxylic acid→diethyl (2-((4-fluoro-2-iodophenyl)amino)-2-oxoethyl)phosphonate→(Z)-N-(2-(diethylamino)ethyl)-5-(3-((4-fluoro-2-iodophenyl)amino)-3-oxoprop-1-en-1-yl)-2,4-dimethyl-1H-pyrrole-3-carboxamide→4-fluoro-2-iodoaniline→2-chloroacetyl chloride→2-chloro-N-(4-fluoro-2-iodophenyl)acetamide→triethyl phosphite

VorolanibOriginator routesteps: 3total yield: 20 mg

5-fluoroindolin-2-one→5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid→(Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid→3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl (Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylate→(S)-3-amino-N,N-dimethylpyrrolidine-1-carboxamide→(S,Z)-N-(1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications	Action
Unibest Nantong cGMP Site	5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid Pharmaceutical Intermediates	On request	On request	On request	—

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